Optimizing Natural Products by Biosynthetic Engineering: Discovery of Nonquinone Hsp90 Inhibitors.
作者
Zhang, Ming-Qiang;Gaisser, Sabine;Nur-E-Alam, Mohammad;Sheehan, Lesley S.;Vousden, William A.;Gaitatzis, Nikolaos;Peck, Gerrard;Coates, Nigel J.;Moss, Steven J.;Radzom, Markus;Foster, Teresa A.;Sheridan, Rose M.;Gregory, Matthew A.;Roe, S. Mark;Prodromou,
[摘要]：A biosynthetic medicinal chem. approach was applied to the optimization of the natural product Hsp90 inhibitor macbecin. By genetic engineering, mutants have been created to produce novel macbecin analogs including a nonquinone compd. that has significantly and reduced toxicity (MTD ?250 mg/kg).
